1) The document discusses adrenergic receptors and neurotransmitters, including alpha and beta receptors.
2) Alpha receptors are further divided into alpha1 and alpha2, while beta receptors are divided into beta1, beta2, and beta3. Each receptor type is located in different parts of the body.
3) Direct-acting adrenergic agonists bind and activate alpha and beta receptors, while indirect agonists stimulate norepinephrine release. Examples of both types are provided.
1. ( ADRENERGIC RECEPTOR AND NEURO TRANSMITER
& DIRECT ACTING ADRENERGIC AGONISTS)
GROUP NAME :-
GROUP MEMBERS :- RUSHABH
HARSHADA
TANVEER
UNDER GUIDANCE OF
- RESPECTED
PRADNYA MA’AM
6. In adrenergic neurons (sympathetic
postganglion), the neurotransmitter released
is norepinephrine, which is also called
noradrenaline.
There are closely related catecholamines
(CAs), that is, adrenaline and dopamine that
has minor effects secreted by adrenal
medulla and in limbic system basal ganglia,
respectively.
8. They are membrane bound G-protein coupled receptors
and classifi ed as α (alpha) and β (beta) adrenoceptors.
α-RECEPTORS :- They are further classified into α1 and α2
. The selective agonist for α1 is phenylephrine and
antagonist is prazosin. α2 receptors are stimulated by
clonidine selectively and antagonized by
yohimbineElicitation of α1 receptors increases
phospholipase C, D, A2, and inositol-
triposphate/diacylglycerol IP3 /DAG which contracts
smooth muscles, genitourinary tracts, and increase the
secretions of glands and in the heart, it increases the force
of contraction. α2 receptor stimulation causes decrease in
cyclic AMP, Ca2+ L type channels, and increases the IP3
/DAG. It decrease the insulin secretion, produces platelet
aggregation, decreases the release of NE as it has auto-
regulation mechanism, and causes the vascular smooth
muscle contraction
9. β-RECEPTORS :- The β receptors are further
subdivided into three subtypes and distributed in the body,
that is, β1 (heart), β2 (bronchi, smooth muscles), and β3
(adipose tissue). Each has a selective agonist and
antagonist. For β1 receptors, the agonist is dobutamine
and antagonists are atenolol and metaprolol. Agonists for
β2 are salbutamol and terbutaline and antagonist is
propranolol. The pharmacology of β receptors indicate the
biochemical increase of adenylcyclase, L-Type calcium
channels increment through β1, causes increase in the
force and rate of contraction of AV nodal conduction
velocity. β2 receptor stimulates bronchodilation through
elicitation of adenylcyclase. β3 stimulation increases
adenylcyclase and causes lipolysis.
10. The drugs are agonist of adernergic alpha
and beta receptor .They bind and stimulate
alpha and beta receptor in specific organ and
give response same as sympathetic
stimulation are called as symphathomimetic
(adernergic) drugs
11. . Direct-acting adrenergic agonists They bind to and
activate α1 , α2 , β1 , and β2 receptors. Naturally occurring
molecules, which bind to these receptors include NE (a
neurotransmitter which binds to α1 , α2 , and β1 receptors),
Epinephrine (a hormone produced in and secreted from the
adrenal medulla, which binds to α1 , α2 , β1 , and β2 receptors, it
is a nonselective adrenergic agonists), and Dopamine (also a
neurotransmitter, which binds to α1 , α2 , and β1 receptors).
Examples of drugs: xylometazoline, phenylephrine, methoxamine.
II. Indirect-acting adrenergic agonists They produce NE-
like actions by stimulating NE release and preventing its reuptake
and produces activation. Example: Tyramine.
III. Dual-acting adrenergic agonists These agents act as
direct and indirect adrenergic agonists (hence, dual-acting). They
bind to adrenergic receptors and stimulate NE release. Examples:
Ephedrine, Amphetamine, Mephenteramine.
12. Chemical name (IUPAC) :- 1-(3- hydroxy phenyl) -2-methlamino ethanol
Properties : It is a white or almost white crystalline powder, freely soluble in
ethanol and water. Phenylephrine differs from adrenaline only by lacking the
4th OH group on the benzene ring, and Adrenergic Drugs subsequently,
resistant to COMT and has predominantly α1 agonist effect. The L-isomer,
causes marked arterial vaso-constriction and is active when given orally.
Uses:- It finds its main use in the relief of nasal congestion and as a mydriatic.
It is also used to prolong the action of local anaesthetics. Uses as vaso-
constriction
Assay: Dissolve the sample in a mixture of 0.1 M hydrochloric acid and
ethanol. Titrate with 0.1 M ethanolic sodium hydroxide and determine the end
point by potentiometric titration.
Dose: By topical, intranasal, adults dose is 2 to 3 drops or 1 or 2 sprays of 0.2
to 0.5% solution; Intramuscular, adults, for mild to moderate hypotension: 2 to
5 mg repeated every 10 to 15 min.
Dosage forms: Phenylephrine eye drops B.P., Phenylephrine injection B.P.
13. Chemical name (IUPAC) :-
2-(4-tert-butyl -2,6-dimethyl benzyl) -2-imidazolin hydrochloride
Properties and uses: It is a potent sympathomimetic agent,
having marked and pronounced α-adrenergic pharmacologic profile. It
is found to act as a vasoconstrictor, when applied topically to mucous
membranes particularly. It is frequently employed as a local vaso-
constrictor for nasal congestion caused by sinusitis or rhinitis.
Dose: By intranasal, 1 drop of a 0.1% solution in adult; or a spray of
0.05% solution.